ATP-competitive inhibitor of MAPK14
Protein target names: MAPK14
Mechanism of action: ATP-competitive inhibitor
In Vitro Validations
In Cell Validations
In Vivo Data
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SERP ratings and comments
This is a selective probe with some off-target activity against p38β; it is able to cross the blood-brain barrier.
(last updated: 23 Jun 2016 )
This probe has a pretty good selectivity towards p38alpha with effects on peripheral blood mononuclear cells (PBMCs) and on a rheumatoid arthritis mouse model.
(last updated: 1 Jul 2016 )
Effective inhibition of p38α should be achievable at concentrations between 50-100 nM. The reported Ki for p38β is 220 nM as determined in α spectrophotometric coupled-enzyme assay using recombinant protein. The Kd for other kinases such as DDR1 is reported to be above 1000 nM. This compound is a fairly selective p38 MAPKα inhibitor with a 20-fold window to p38 MAPKβ based on assessment in an activity assay. It is also useful as an in vivo probe.
(last updated: 3 Jul 2017 )